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Special Issue "Anti-Infective Agents"

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A special issue of Molecules (ISSN 1420-3049).

Deadline for manuscript submissions: closed (31 March 2010)

Special Issue Editors

Guest Editor
Prof. Dr. Paul Cos

Laboratory of Microbiology, Parasitology and Hygiene (LMPH), Department of Pharmaceutical Sciences, Faculty of Pharmaceutical, Biomedical and Veterinary Sciences Antwerp University, campus drie eiken, building S, office 7.26 Universiteitsplein 1, B-2610 Antwerp, Belgium
Website | E-Mail
Interests: anti-infective agents; biofilm; bacterial virulence; oxidative stress; antibacterial; antifungal; antiparasitic and antiviral
Guest Editor
Prof. Dr. Mark Hamann

Department of Pharmacognosy and The National Center for the Development of Natural Products, University of Mississippi, USA
Website | E-Mail
Interests: natural products; antiinfectives; anticancer agents; NMR spectroscopy; marine ecology; synthesis of natural products; biosynthesis

Special Issue Information

Dear Colleagues,

Despite the tremendous progress in human medicine, infectious diseases represent one of the greatest challenges to mankind in the 21st century. According to WHO, infectious diseases account for nearly a third of global deaths. AIDS, malaria, tuberculosis and respiratory infections were among the top eight leading causes of death in 2004. The burden of infectious diseases falls particularly on the less developed countries due to the relative unavailability of medicines and the emergence of widespread drug resistance. In developing countries, a high infectious disease burden commonly co-exists with rapid emergence and spread of microbial resistance. The growing threat of emerging diseases such as SARS and influenza A (H1N1) has served as a wake-up call to public health services, pharmaceutical industry and academia.
Because the evolution of drug resistance is likely to compromise every drug in time, research on new anti-infective agents must be continued and all possible strategies should be explored. Besides small molecules from medicinal chemistry, natural products are still major sources of innovative therapeutic agents for various conditions, including infectious diseases.
This special issue welcomes research articles and comprehensive reviews addressing the discovery and/or development of anti-infective agents.

Prof. Dr. Paul Cos
Prof. Dr. Mark Hamann
Guest Editors

Keywords

  • anti-infectives
  • biofilm
  • bacterial virulence
  • oxidative stress
  • antibacterial
  • antifungal
  • antiparasitic
  • antiviral
  • screening
  • small molecules
  • natural products

Related Special Issue

Published Papers (5 papers)

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Research

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Open AccessArticle Antifungal Effect of (+)-Pinoresinol Isolated from Sambucus williamsii
Molecules 2010, 15(5), 3507-3516; doi:10.3390/molecules15053507
Received: 9 April 2010 / Revised: 6 May 2010 / Accepted: 11 May 2010 / Published: 14 May 2010
Cited by 19 | PDF Full-text (631 KB)
Abstract
In this study, we investigated the antifungal activity and mechanism of action of (+)-pinoresinol, a biphenolic compound isolated from the herb Sambucus williamsii,used in traditional medicine. (+)-Pinoresinol displays potent antifungal properties without hemolytic effects on human erythrocytes. To understand the antifungal mechanism
[...] Read more.
In this study, we investigated the antifungal activity and mechanism of action of (+)-pinoresinol, a biphenolic compound isolated from the herb Sambucus williamsii,used in traditional medicine. (+)-Pinoresinol displays potent antifungal properties without hemolytic effects on human erythrocytes. To understand the antifungal mechanism of (+)-pinoresinol, we conducted fluorescence experiments on the human pathogen Candida albicans. Fluorescence analysis using 1,6-diphenyl-1,3,5-hexatriene (DPH) indicated that the (+)-pinoresinol caused damage to the fungal plasma membrane. This result was confirmed by using rhodamine-labeled giant unilamellar vesicle (GUV) experiments. Therefore, the present study indicates that (+)-pinoresinol possesses fungicidal activities and therapeutic potential as an antifungal agent for the treatment of fungal infectious diseases in humans. Full article
(This article belongs to the Special Issue Anti-Infective Agents)

Review

Jump to: Research

Open AccessReview Discovery and Development of Anti-HBV Agents and Their Resistance
Molecules 2010, 15(9), 5878-5908; doi:10.3390/molecules15095878
Received: 4 August 2010 / Revised: 24 August 2010 / Accepted: 26 August 2010 / Published: 27 August 2010
Cited by 24 | PDF Full-text (642 KB)
Abstract
Hepatitis B virus (HBV) infection is a prime cause of liver diseases such as hepatitis, cirrhosis and hepatocellular carcinoma. The current drugs clinically available are nucleot(s)ide analogues that inhibit viral reverse transcriptase activity. Most drugs of this class are reported to have viral
[...] Read more.
Hepatitis B virus (HBV) infection is a prime cause of liver diseases such as hepatitis, cirrhosis and hepatocellular carcinoma. The current drugs clinically available are nucleot(s)ide analogues that inhibit viral reverse transcriptase activity. Most drugs of this class are reported to have viral resistance with breakthrough. Recent advances in methods for in silico virtual screening of chemical libraries, together with a better understanding of the resistance mechanisms of existing drugs have expedited the discovery and development of novel anti-viral drugs. This review summarizes the current status of knowledge about and viral resistance of HBV drugs, approaches for the development of novel drugs as well as new viral and host targets for future drugs. Full article
(This article belongs to the Special Issue Anti-Infective Agents)
Figures

Open AccessReview Conazoles
Molecules 2010, 15(6), 4129-4188; doi:10.3390/molecules15064129
Received: 4 May 2010 / Accepted: 7 June 2010 / Published: 9 June 2010
Cited by 38 | PDF Full-text (510 KB)
Abstract
This review provides a historical overview of the analog based drug discovery of miconazole and its congeners, and is focused on marketed azole antifungals bearing the generic suffix “conazole”. The antifungal activity of miconazole, one of the first broad-spectrum antimycotic agents has been
[...] Read more.
This review provides a historical overview of the analog based drug discovery of miconazole and its congeners, and is focused on marketed azole antifungals bearing the generic suffix “conazole”. The antifungal activity of miconazole, one of the first broad-spectrum antimycotic agents has been mainly restricted to topical applications. The attractive in vitro antifungal spectrum was a starting point to design more potent and especially orally active antifungal agents such as ketoconazole, itraconazole, posaconazole, fluconazole and voriconazole. The chemistry, in vitro and in vivo antifungal activity, pharmacology, and clinical applications of these marketed conazoles has been described. Full article
(This article belongs to the Special Issue Anti-Infective Agents)
Figures

Open AccessReview Chemistry and Structure-Activity Relationship of the Styrylquinoline-Type HIV Integrase Inhibitors
Molecules 2010, 15(5), 3048-3078; doi:10.3390/molecules15053048
Received: 2 March 2010 / Revised: 8 April 2010 / Accepted: 12 April 2010 / Published: 27 April 2010
Cited by 28 | PDF Full-text (776 KB)
Abstract
In spite of significant progress in anti-HIV-1 therapy, current antiviral chemo-therapy still suffers from deleterious side effects and emerging drug resistance. Therefore, the development of novel antiviral drugs remains a crucial issue for the fight against AIDS. HIV-1 integrase is a key enzyme
[...] Read more.
In spite of significant progress in anti-HIV-1 therapy, current antiviral chemo-therapy still suffers from deleterious side effects and emerging drug resistance. Therefore, the development of novel antiviral drugs remains a crucial issue for the fight against AIDS. HIV-1 integrase is a key enzyme in the replication cycle of the retrovirus since it catalyzes the integration of the reverse transcribed viral DNA into the chromosomal DNA. Efforts to develop anti-integrase drugs started during the early nineties, culminating with the recent approval of Raltegravir. The discovery and the development of the styrylquinoline inhibitor class was an important step in the overall process. In this review we have described the key synthetic issues and the structure-activity relationship of this family of integrase inhibitors. Crystallographic and docking studies that shed light on their mechanism of action are also examined. Full article
(This article belongs to the Special Issue Anti-Infective Agents)
Figures

Open AccessReview Arginine as a Synergistic Virucidal Agent
Molecules 2010, 15(3), 1408-1424; doi:10.3390/molecules15031408
Received: 14 January 2010 / Revised: 11 February 2010 / Accepted: 4 March 2010 / Published: 8 March 2010
Cited by 3 | PDF Full-text (512 KB)
Abstract
Development of effective and environmentally friendly disinfectants, or virucidal agents, should help prevent the spread of infectious diseases through human contact with contaminated surfaces. These agents may also be used, if non-toxic to cells and tissues, as chemotherapeutic agents against infectious diseases. We
[...] Read more.
Development of effective and environmentally friendly disinfectants, or virucidal agents, should help prevent the spread of infectious diseases through human contact with contaminated surfaces. These agents may also be used, if non-toxic to cells and tissues, as chemotherapeutic agents against infectious diseases. We have shown that arginine has a synergistic effect with a variety of virucidal conditions, namely acidic pH and high temperature, on virus inactivation. All of these treatments are effective, however, at the expense of toxicity. The ability of arginine to lower the effective threshold of these parameters may reduce the occurrence of potential toxic side effects. While it is clear that arginine can be safely used, the mechanism of its virus inactivation has not yet been elucidated. Here we examine the damages that viruses suffer from various physical and chemical stresses and their relations to virus inactivation and aggregation. Based on the relationship between the stress-induced structural damages and the infectivity of a virus, we will propose several plausible mechanisms describing the effects of arginine on virus inactivation using the current knowledge of aqueous arginine solution properties. Full article
(This article belongs to the Special Issue Anti-Infective Agents)

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